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Identification of Histone Peptide Binding Specificity and Small-Molecule Ligands for the TRIM33α and TRIM33β Bromodomains.
ACS Chem Biol. 2022 Oct 21;17(10):2753-2768. doi: 10.1021/acschembio.2c00266. Epub 2022 Sep 13.
ACS Chem Biol. 2022.
PMID: 36098557
Free PMC article.
Absolute Alchemical Free Energy Calculations for Ligand Binding: A Beginner's Guide.
Aldeghi M, Bluck JP, Biggin PC.
Aldeghi M, et al. Among authors: bluck jp.
Methods Mol Biol. 2018;1762:199-232. doi: 10.1007/978-1-4939-7756-7_11.
Methods Mol Biol. 2018.
PMID: 29594774
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BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability.
Jennings LE, Schiedel M, Hewings DS, Picaud S, Laurin CMC, Bruno PA, Bluck JP, Scorah AR, See L, Reynolds JK, Moroglu M, Mistry IN, Hicks A, Guzanov P, Clayton J, Evans CNG, Stazi G, Biggin PC, Mapp AK, Hammond EM, Humphreys PG, Filippakopoulos P, Conway SJ.
Jennings LE, et al. Among authors: bluck jp.
Bioorg Med Chem. 2018 Jul 15;26(11):2937-2957. doi: 10.1016/j.bmc.2018.05.003. Epub 2018 May 15.
Bioorg Med Chem. 2018.
PMID: 29776834
Free article.
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Fragment-Based Identification of Ligands for Bromodomain-Containing Factor 3 of Trypanosoma cruzi.
Laurin CMC, Bluck JP, Chan AKN, Keller M, Boczek A, Scorah AR, See KFL, Jennings LE, Hewings DS, Woodhouse F, Reynolds JK, Schiedel M, Humphreys PG, Biggin PC, Conway SJ.
Laurin CMC, et al. Among authors: bluck jp.
ACS Infect Dis. 2021 Aug 13;7(8):2238-2249. doi: 10.1021/acsinfecdis.0c00618. Epub 2020 Nov 17.
ACS Infect Dis. 2021.
PMID: 33203208
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Controlling Intramolecular Interactions in the Design of Selective, High-Affinity Ligands for the CREBBP Bromodomain.
Brand M, Clayton J, Moroglu M, Schiedel M, Picaud S, Bluck JP, Skwarska A, Bolland H, Chan AKN, Laurin CMC, Scorah AR, See L, Rooney TPC, Andrews KH, Fedorov O, Perell G, Kalra P, Vinh KB, Cortopassi WA, Heitel P, Christensen KE, Cooper RI, Paton RS, Pomerantz WCK, Biggin PC, Hammond EM, Filippakopoulos P, Conway SJ.
Brand M, et al. Among authors: bluck jp.
J Med Chem. 2021 Jul 22;64(14):10102-10123. doi: 10.1021/acs.jmedchem.1c00348. Epub 2021 Jul 13.
J Med Chem. 2021.
PMID: 34255515
Free PMC article.
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Mutate and Conjugate: A Method to Enable Rapid In-Cell Target Validation.
Thomas AM, Serafini M, Grant EK, Coombs EAJ, Bluck JP, Schiedel M, McDonough MA, Reynolds JK, Lee B, Platt M, Sharlandjieva V, Biggin PC, Duarte F, Milne TA, Bush JT, Conway SJ.
Thomas AM, et al. Among authors: bluck jp.
ACS Chem Biol. 2023 Nov 17;18(11):2405-2417. doi: 10.1021/acschembio.3c00437. Epub 2023 Oct 24.
ACS Chem Biol. 2023.
PMID: 37874862
Free PMC article.
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Prioritizing Small Sets of Molecules for Synthesis through in-silico Tools: A Comparison of Common Ranking Methods.
Breznik M, Ge Y, Bluck JP, Briem H, Hahn DF, Christ CD, Mortier J, Mobley DL, Meier K.
Breznik M, et al. Among authors: bluck jp.
ChemMedChem. 2023 Jan 3;18(1):e202200425. doi: 10.1002/cmdc.202200425. Epub 2022 Nov 29.
ChemMedChem. 2023.
PMID: 36240514
Free PMC article.
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Discovery and characterization of orally bioavailable 4-chloro-6-fluoroisophthalamides as covalent PPARG inverse-agonists.
Orsi DL, Ferrara SJ, Siegel S, Friberg A, Bouché L, Pook E, Lienau P, Bluck JP, Lemke CT, Akcay G, Stellfeld T, Meyer H, Pütter V, Holton SJ, Korr D, Jerchel-Furau I, Pantelidou C, Strathdee CA, Meyerson M, Eis K, Goldstein JT.
Orsi DL, et al. Among authors: bluck jp.
Bioorg Med Chem. 2023 Jan 15;78:117130. doi: 10.1016/j.bmc.2022.117130. Epub 2022 Dec 13.
Bioorg Med Chem. 2023.
PMID: 36542958
Free article.
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